Sometimes finding a potent inhibitor or agonist for a particular biological target is the most difficult part of drug development. Often, however, getting the drug to its target in the body is a bigger challenge than achieving high potency or avoiding undesirable off-target effects. This is especially so for oral drug delivery, which is generally the preferred route because of its relative convenience, but it can be a problem for other routes of administration as well. Low solubility of active pharmaceutical ingredients limits absorption, so getting the drug into solution and keeping it there is key. Formulation scientists have a wide range of ways they can address solubility problems, many of which involve exploiting kinetic aspects of dissolution, precipitation and crystallization. One is to create and sustain supersaturated solutions, thereby enhancing absorption and bioavailability. Another is to impede crystallization. The physical chemistry underlying these and other such approaches will be outlined in this talk, as will the use of mechanistic and statistical models to aid in getting around the sort of thermodynamic solubility problems often encountered in drug development.<br/>

Anticipating and addressing solubility and precipitation problems computationally

2019 Fall National Meeting

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